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使用场刺激右猫心房研究酚妥拉明对突触前α2-肾上腺素能受体和突触前多巴胺受体的拮抗特性。

Antagonist properties of phentolamine at both presynaptic alpha 2-adrenoceptors and presynaptic dopamine receptors using field stimulated right cat atria.

作者信息

Koons J C, Flynn J R, Long J P

出版信息

Eur J Pharmacol. 1983 Apr 8;88(4):311-7. doi: 10.1016/0014-2999(83)90581-2.

Abstract

Phentolamine, which is considered a specific alpha-adrenoceptor antagonist, was tested for antagonist properties at presynaptic dopamine receptors and presynaptic alpha 2-adrenoceptors present on sympathetic nerve terminals in isolated right cat atria. Field stimulation induced a transient tachycardia which was inhibited by stimulation of presynaptic dopamine receptors using apomorphine or by stimulation of presynaptic alpha 2-adrenoceptors using clonidine. The presynaptic inhibitory effects of apomorphine were competitively antagonized by sulpiride, which is considered a specific dopamine receptor antagonist, and by phentolamine and yohimbine which are considered alpha-adrenoceptor antagonists. The presynaptic inhibitory effects of clonidine were competitively antagonized by phentolamine and yohimbine but not by sulpiride. pA2 values for phentolamine against apomorphine and phentolamine against clonidine suggest that phentolamine may be an antagonist at both presynaptic dopamine receptors and presynaptic alpha 2-adrenoceptors.

摘要

酚妥拉明被认为是一种特异性α-肾上腺素能受体拮抗剂,在离体右心房猫中,对存在于交感神经末梢的突触前多巴胺受体和突触前α2-肾上腺素能受体的拮抗特性进行了测试。场刺激诱发短暂性心动过速,使用阿扑吗啡刺激突触前多巴胺受体或使用可乐定刺激突触前α2-肾上腺素能受体可抑制该心动过速。阿扑吗啡的突触前抑制作用被被认为是特异性多巴胺受体拮抗剂的舒必利以及被认为是α-肾上腺素能受体拮抗剂的酚妥拉明和育亨宾竞争性拮抗。可乐定的突触前抑制作用被酚妥拉明和育亨宾竞争性拮抗,但不被舒必利拮抗。酚妥拉明针对阿扑吗啡和酚妥拉明针对可乐定的pA2值表明,酚妥拉明可能是突触前多巴胺受体和突触前α2-肾上腺素能受体的拮抗剂。

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